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Discovery of SHR9352: A Highly Potent G Protein-Biased μ-Opioid Receptor Agonist
[Image: see text] Recently, targeting the G protein-biased signaling has emerged as an attractive therapeutic strategy for treating severe acute pain with the potential to reduce the side effect of the traditional opioid drug. Herein, we describe the discovery of a highly potent G protein-biased μ-o...
| Autores principales: | , , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
American Chemical Society
2017
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| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6645658/ https://www.ncbi.nlm.nih.gov/pubmed/31457439 http://dx.doi.org/10.1021/acsomega.7b01452 |
| _version_ | 1783437511288160256 |
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| author | Li, Xin He, Wei Chen, Yang Yang, Guimei Wan, Hong Zhang, Lei Hu, Qiyue Feng, Jun Zhang, Zhigao He, Feng Bai, Chang Zhang, Lianshan You, Li Tao, Weikang |
| author_facet | Li, Xin He, Wei Chen, Yang Yang, Guimei Wan, Hong Zhang, Lei Hu, Qiyue Feng, Jun Zhang, Zhigao He, Feng Bai, Chang Zhang, Lianshan You, Li Tao, Weikang |
| author_sort | Li, Xin |
| collection | PubMed |
| description | [Image: see text] Recently, targeting the G protein-biased signaling has emerged as an attractive therapeutic strategy for treating severe acute pain with the potential to reduce the side effect of the traditional opioid drug. Herein, we describe the discovery of a highly potent G protein-biased μ-opioid receptor (MOR) agonist, SHR9352. This novel molecule exhibited excellent MOR activity and limited β-arrestin recruitment, as well as a high selectivity over κ-opioid receptor and δ-opioid receptor demonstrated robust in vivo efficacy and displayed favorable pharmacokinetic properties across species. |
| format | Online Article Text |
| id | pubmed-6645658 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2017 |
| publisher | American Chemical Society |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-66456582019-08-27 Discovery of SHR9352: A Highly Potent G Protein-Biased μ-Opioid Receptor Agonist Li, Xin He, Wei Chen, Yang Yang, Guimei Wan, Hong Zhang, Lei Hu, Qiyue Feng, Jun Zhang, Zhigao He, Feng Bai, Chang Zhang, Lianshan You, Li Tao, Weikang ACS Omega [Image: see text] Recently, targeting the G protein-biased signaling has emerged as an attractive therapeutic strategy for treating severe acute pain with the potential to reduce the side effect of the traditional opioid drug. Herein, we describe the discovery of a highly potent G protein-biased μ-opioid receptor (MOR) agonist, SHR9352. This novel molecule exhibited excellent MOR activity and limited β-arrestin recruitment, as well as a high selectivity over κ-opioid receptor and δ-opioid receptor demonstrated robust in vivo efficacy and displayed favorable pharmacokinetic properties across species. American Chemical Society 2017-12-28 /pmc/articles/PMC6645658/ /pubmed/31457439 http://dx.doi.org/10.1021/acsomega.7b01452 Text en Copyright © 2017 American Chemical Society This is an open access article published under an ACS AuthorChoice License (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes. |
| spellingShingle | Li, Xin He, Wei Chen, Yang Yang, Guimei Wan, Hong Zhang, Lei Hu, Qiyue Feng, Jun Zhang, Zhigao He, Feng Bai, Chang Zhang, Lianshan You, Li Tao, Weikang Discovery of SHR9352: A Highly Potent G Protein-Biased μ-Opioid Receptor Agonist |
| title | Discovery of SHR9352: A Highly Potent G Protein-Biased μ-Opioid
Receptor Agonist |
| title_full | Discovery of SHR9352: A Highly Potent G Protein-Biased μ-Opioid
Receptor Agonist |
| title_fullStr | Discovery of SHR9352: A Highly Potent G Protein-Biased μ-Opioid
Receptor Agonist |
| title_full_unstemmed | Discovery of SHR9352: A Highly Potent G Protein-Biased μ-Opioid
Receptor Agonist |
| title_short | Discovery of SHR9352: A Highly Potent G Protein-Biased μ-Opioid
Receptor Agonist |
| title_sort | discovery of shr9352: a highly potent g protein-biased μ-opioid
receptor agonist |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6645658/ https://www.ncbi.nlm.nih.gov/pubmed/31457439 http://dx.doi.org/10.1021/acsomega.7b01452 |
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